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Biologically privileged fused pyrimidine spirocycles were synthesized via a metal‐free three‐component cascade reaction utilizing mercapto/aza lactam active methylene compounds. This rapid and efficient one‐pot operation quickly delivered seven different polycyclic and spirocyclic scaffolds such as pyranothiazolopyrimidine, benzothiazolopyranopyrimidine, pyranotriazolopyrimidine, benzoimidazolopyranopyrimidine, spiroindolinepyranothiazolopyrimidine, spirobenzothiazolopyranopyrimidineindoline, and spirobenzo‐imidazolopyranopyrimidineindoline at room temperature with excellent regio/chemoselectivity.

An eco‐friendly reaction protocol was developed for the synthesis of heterocyclic hybrid scaffolds through bioisosteric replacement and scaffold hopping approach. The isosteric analogues of salicylaldehyde were designed, identified/synthesized and employed in a three component reaction to afford bioisosteric analogues of 4‐aryl‐4H‐chromenes. Thus central core swapping of benzene‐pyridine/pyrazole ring on 4‐aryl‐4H‐chromenes was achieved under simple one‐pot reaction conditions and easy work‐up. Docking studies show that almost all the compounds possess good binding affinities at the colchicine binding site of tubulin.